Pyridazinoquinolinetriones as NMDA glycine-site antagonists with oral antinociceptive activity in a model of neuropathic pain

…, CL Horchler, M Murphy, RA Urbanek…

文献索引：Bare, Thomas M.; Brown, Dean G.; Horchler, Carey L.; Murphy, Megan; Urbanek, Rebecca A.; Alford, Vernon; Barlaam, Christine; Dyroff, Martin C.; Empfield, James B.; Forst, Janet M.; Herzog, Keith J.; Keith, Richard A.; Kirschner, Alan S.; Lee, Chi-Ming C.; Lewis, Joseph; McLaren, Frances M.; Neilson, Kathy L.; Steelman, Gary B.; Trivedi, Shephali; Vacek, Edward P.; Xiao, Wenhua Journal of Medicinal Chemistry, 2007 , vol. 50, # 13 p. 3113 - 3131

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被引用次数: 10

摘要

A series of 7-chloro-2, 3-dihydro-2-[1-(pyridinyl) alkyl]-pyridazino [4, 5-b] quinoline-1, 4, 10 (5 H)-triones were synthesized and found to have potent activity at the glycine site of the NMDA receptor. In some cases, these compounds possessed poor aqueous solubility that may have contributed to poor rat oral bioavailability. Subsequently, compounds have been identified with improved aqueous solubility and oral bioavailability. Several of these ...